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Benzimidazole derivatives as Kinase Inhibitors
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a technology of kinase inhibitors and benzimidazole, which is applied in the field ofbenzimidazole derivatives, can solve the problems of poor prognosis, poor association of presence, and the inability of pim-2 to prevent apoptosis upon glucose deprivation
Active Publication Date: 2016-07-12
SELVITA SA
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The present invention relates to a compound of formula (I) and its pharmaceutically acceptable salt, which exhibits strong inhibitory activity against PIM1-3 and DYRK kinases. The compound has good solubility and can be easily administered as a drug.
Problems solved by technology
Constitutively activating internal tandem duplication (ITD) mutations of the receptortyrosine kinase FLT3 play an important role in leukemogenesis, and their presence is associated with poor prognosis in AML.
It was also found that protection against apoptosis by PIM-2 is glucose-dependent, so liver cells growing in vivo, surrounded by high glucose and growth factors concentration have favorable conditions to express PIM-2, however PIM-2 was unable to prevent apoptosis upon glucose deprivation.
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[0076]The inventors of the present invention inter alia succeeded in identifying new compounds which efficiently inhibit PIM1-3- and DYRK1A-kinases. The compounds of the present invention may thus be particularly used in the treatment of cancer, autoimmune diseases and inflammatory diseases.
[0077]Before some of the embodiments of the present invention are described in more detail, the following definitions are introduced.
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[0078]As used in the specification and the claims, the singular forms of “a” and “an” also include the corresponding plurals unless the context clearly dictates otherwise. The same applies for plural forms used herein, which also include the singular forms unless the context clearly dictates otherwise.
[0079]The terms “about” and “approximately” in the context of the present invention denotes an interval of accuracy that a person skilled in the art will understand to still ensure the technical effect of the feature in question. The te...
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Abstract
The present invention relates to derivatives of benzimidazoles of formula (I) as disclosed herein as well as pharmaceutical compositions comprising said derivatives. The derivates according to the present invention are serine / threonine and tyrosinekinase-inhibitors, particularly of PIM1-3- and DYRK1A-kinases and may particularly be used in the treatment of diseases linked to these kinases, such as e.g. leukemias, lymphomas, solid tumors and autoimmune disorders.
Description
FIELD OF THE INVENTION[0001]The present invention relates to novel benzimidazole derivatives and pharmaceutically acceptable salts thereof. Such derivatives are potent inhibitors of certain serine / threonine and tyrosine kinases and in particular of PIM1-3- and DYRK1A-kinases. The present invention further relates to pharmaceutical compositions comprising such derivatives, wherein the pharmaceutical compositions are particularly useful in the treatment of PIM1-3-kinase- and DYRK1A-kinase-related disorders such as cancers (in particular leukemias, lymphomas and solid tumors), autoimmune diseases, inflammatory diseases and neurodegenerative disorders.BACKGROUND OF THE INVENTION[0002]Kinases are enzymes that modify other proteins by chemically adding phosphate groups to them (a process called phosphorylation). Phosphorylation of the targeted proteins results in a functional change of their activity but also can modify association with other proteins, trafficking and subcellular localiza...
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Application Information
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